YL5084
YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner.
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- CAS. Nr.: 2440199-73-3
- Formel: C35H36N8O2
- Molecular Weight:600.71
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
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JNK2 70 nM (IC50) |
JNK3 84 nM (IC50) |
JNK1 2173 nM (IC50) |
YL5084 (0.001-100 μM; 72 h) displays dose-dependent antiproliferative effects with GR50 values of 200-300 nM in MM.1S cells[1].
YL5084 (0.5, 2.5 μM; 24 h) induces apoptosis[1].
YL5084 displays weaker inhibition against PIKFYVE (KD=5000 nM in a KdELECT binding assay) in KINOMEscan[1].
YL5084 has moderate metabolic stability in human and mice microsomes with half-lives of 16 and 11 min, respectively [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Multiple myeloma (MM) cell lines
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Concentration:0.001-100 μM
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Incubation Time:72 h
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Result:Displayed dose-dependent antiproliferative effects with GR50 values of 200-300 nM.
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Cell Line:MM.1S cells
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Concentration:0.5, 2.5 μM
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Incubation Time:24 h
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Result:Induced apoptosis as evidenced by an increased level of PARP cleavage, an increased level of cleavage of caspase 3, and an increased level of Annexin V/PI staining.
Chemical Information
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CAS. Nr. 2440199-73-3
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Molecular Weight 600.71
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Formel C35H36N8O2
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SMILES
O=C(C1=CC=C(C=C1)NC(/C=C/CN(C)C)=O)N(C[C@@H]2C)C[C@H]2NC3=NC=CC(C4=C(C=CC=C5)N5N=C4C6=CC=CC=C6)=N3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
YL5084 Related Classifications
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